Mdivi 1
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Mdivi-1是一种细胞渗透性的线粒体分裂DRP1(发动蛋白相关GTP酶)和线粒体分裂发动蛋白I(Dnm1)选择性抑制剂,属于大GTP酶发动蛋白家族,可以调控线粒体分裂。
体外:Mdivi-1是最有效的抑制剂,选择性抑制线粒体DRP1介导的分裂发动蛋白,从而减少酵母和哺乳动物细胞中的线粒体分裂。Mdivi-1有效阻止Bid激活的Bax/Bak依赖性细胞色素C从线粒体中释放[1]。
体内:Mdivi-1治疗可以阻止缺血性视网膜的凋亡性细胞死亡,并于缺血后2周显著增加RGC细胞存活。此外,Mdivi-1治疗不会影响Drp1蛋白表达的增加,但可以显著下调GFAP蛋白表达[2]。
临床试验:目前没有可用的临床数据。
参考文献:
[1] Cassidy-Stone A, Chipuk JE, Ingerman E, Song C, Yoo C, Kuwana T, Kurth MJ, Shaw JT, Hinshaw JE, Green DR, Nunnari J. Chemical inhibition of the mitochondrial division dynamin reveals its role in Bax/Bak-dependent mitochondrial outer membrane permeabilization. Dev Cell. 2008;14(2):193-204.
[2] Park SW, Kim KY, Lindsey JD, Dai Y, Heo H, Nguyen DH, Ellisman MH, Weinreb RN, Ju WK. A selective inhibitor of drp1, mdivi-1, increases retinal ganglion cell survival in acute ischemic mouse retina. Invest Ophthalmol Vis Sci. 2011;52(5):2837-43.
- 2. Weiwei Qin, Xiyang Tong, et al. "Preservation of mitochondrial homeostasis is responsible for the ameliorative effects of Suhuang antitussive capsule on non-resolving inflammation via inhibition of NF-κB signaling and NLRP3 inflammasome activation." J Ethnopharmacol. 2021 May 10;271:113827. PMID: 33460751
- 1. Raja Gopal Reddy Mooli, Dhanunjay Mukhi, et al. "An indispensable role for dynamin-related protein 1 in beige and brown adipogenesis." J Cell Sci. 2020 Sep 15;133(18):jcs247593. PMID: 32843579
- 3. Qin W, Wu X, et al. "Suhuang antitussive capsule inhibits NLRP3 inflammasome activation and ameliorates pulmonary dysfunction via suppression of endoplasmic reticulum stress in cough variant asthma." Biomed Pharmacother. 2019 Jul 14;118:109188. PMID: 31315072
- 4. Chien L, Liang MZ, et al. "Mitochondrial therapy promotes regeneration of injured hippocampal neurons." Biochim Biophys Acta. 2018 Jun 15. pii: S0925-4439(18)30216-3. PMID: 29913215
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 353.22 |
Cas No. | 338967-87-6 |
Formula | C15H10Cl2N2O2S |
Solubility | insoluble in H2O; insoluble in EtOH; ≥17.65 mg/mL in DMSO |
Chemical Name | 3-(2,4-dichloro-5-methoxyphenyl)-2-sulfanylidene-1H-quinazolin-4-one |
SDF | Download SDF |
Canonical SMILES | COC1=C(C=C(C(=C1)N2C(=O)C3=CC=CC=C3NC2=S)Cl)Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
具有温度敏感性fzo1-1等位基因的酵母细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于17.7 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
50 μM |
应用 |
Mdivi-1(50 μM)通过衰减Drp1的自组装抑制哺乳动物COS细胞中的线粒体分裂。Mdivi-1(50 μM)减弱凋亡过程中哺乳动物的线粒体分裂和Drp1自组装。FACS分析显示,Mdivi-1显著抑制STS诱导的非坏死细胞的膜联蛋白V染色,表明mdivi-1抑制细胞凋亡。 |
动物实验 [2]: | |
动物模型 |
C57BL/6小鼠 |
给药剂量 |
腹腔注射,50 mg/kg,60分钟 |
应用 |
Mdivi-1显著提高RGC存活率,中心区约为54%,中部为58%,外周区为48%。Mdivi-1治疗12小时,明显降低缺血性视网膜中的GFAP蛋白表达。Mdivi-1不改变平均动脉血压、体重、动物的外观或行为。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Cassidy-Stone A, Chipuk J E, Ingerman E, et al. Chemical inhibition of the mitochondrial division dynamin reveals its role in Bax/Bak-dependent mitochondrial outer membrane permeabilization[J]. Developmental cell, 2008, 14(2): 193-204. [2]. Park S W, Kim K Y, Lindsey J D, et al. A selective inhibitor of drp1, mdivi-1, increases retinal ganglion cell survival in acute ischemic mouse retina[J]. Investigative ophthalmology & visual science, 2011, 52(5): 2837-2843. |
Description | Mdivi 1是一种细胞渗透性的线粒体分裂发动蛋白相关GTP酶(DRP1)和线粒体分裂发动蛋白I(Dnm1)选择性抑制剂。 | |||||
靶点 | DRP1 | Dnm1 | ||||
IC50 | 1 - 10 ?M |
质量控制和MSDS
- 批次: